Abstract: A process of preparing camptothecin derivatives of formula 1 is disclosed

Abstract: A pharmaceutical composition comprising a cyclosporin solid-state microemulsion is disclosed. In a preferred embodiment, the composition comprises a cyclosporin microemulsion dispersed in an enteric carrier. The composition does not dissolve in external phases such as artificial gastric fluid, but dissolves rapidly in artificial intestinal fluid, whereby it releases the cyclosporin microemulsion, providing rapid delivery of cyclosporin. The composition effectively maintains a therapeutic blood concentration of cyclosporin with once a day dosing, providing for convenience of administration and avoiding adverse effects induced by increasing peak blood cyclosporin concentrations associated with conventional cyclosporin formulations.

Abstract: Camptothecin derivatives and pharmaceutically acceptable salts thereof, its manufacturing method and an antineoplastic agent containing it. The camptothecin derivatives are modified in B-ring and E-ring and show improved water solubility and enhanced antineoplastic effect.

Abstract: Intermediates for the synthesis of camptothecin of the formula II wherein: R1 is —(CH2)2NR1R2, where R1 is an amino protecting group and R2 is C2-C5 alkyl, hydroxyethyl or acetoxyethyl group, and of the formula III wherein: n is 1 or 2; R3 is hydrogen or —OR4, where R4 is hydrogen, —COR5, —CONHR6 or CH2OR7, where R5 is methyl or —CH2OCH3, R6 is isopropyl, phenyl or —CH2CH2Cl, and R7 is methyl, ethyl or —CH2CH2OCH3; with the proviso that when n is 2, R3 is not hydrogen.

Abstract: According to the present invention, provided are novel nucleoside derivatives having antiviral activity, in particular, anti-HBV (anti-Hepatitis-B Virus) activity, represented by general formula (I), wherein R.sub.1 represents hydrogen, phosphate, phosphonate, alkyl or acyl; R.sub.2 represents alkoxy or halogen; R.sub.3 represents substituted or non-substituted pyrimidine or purine base; and X represents O, S, SO or SO.sub.2 ; pharmaceutically acceptable salts thereof, and processes thereof. As the compound (I) has two or more asymmetric carbon atoms, all possible stereoisomers and mixtures thereof are included in the scope of the present invention.

Abstract: The present invention relates to a microemulsion preconcentrate composition comprising (1) cyclosporin as an active component; (2) alkyl ester of polycarboxylic acid and/or carboxylic acid ester of polyols as a lipophilic solvent; (3) oil; and (4) surfactant. The composition according to the present invention is characterized in that it dissolves in an external phase such as water, artificial gastric fluid and artificial intestinal fluid by controlling the mixing ratio of the components thereby to get the microemulsion form of inner phase diameter of 100 nm or below. The composition according to the present invention can be formulated as the dosage form of a soft capsule, a hard capsule sealed with a gelatin banding at the conjugated portion, or an oral liquid preparation for oral administration.

Abstract: The present invention is related to a new analgesic composition of acetaminophen targeting decreasing of liver toxicity and releasing of hangover, which comprises aspartic acid promoting alcohol metabolism and methionine alleviating liver toxicity of acetaminophen. The analgesic combination preparation according to the present invention showed same analgesic and excellent protection effect against liver toxicity compared with the single preparation of acetaminophen, and decreased the blood concentration of alcohol and acetaldehyde causing hangover through improving metabolism rates of them. The combination preparation according to the present invention, therefore, is coincident with ideal new analgesic composition of acetaminophen having a minimized side effect and a hangover releasing effect.

Abstract: Nucleoside derivatives represented by formula (I); ##STR1## wherein, R.sub.1 represents hydrogen, phosphate or phosphonate group, R.sub.2 represents substituted or unsubstituted pyrimidine or purine base, and Z represents S, SO, SO.sub.2, O or C; or pharmaceutically acceptable salts thereof. Compound (I) can be obtained by reacting a compound of the formula (II); ##STR2## wherein, R.sub.7 represents hydrogen or hydroxy-protecting group, L represents aromatic or nonaromatic acyl, halide or alkoxy, and Z represents S, SO, SO.sub.2, O or C, with a base.

Abstract: The present invention relates to a microemulsion preconcentrate composition comprising (1) cyclosporin as an active component; (2) alkyl ester of polycarboxylic acid and/or carboxylic acid ester of polyols as a lipophilic solvent; (3) oil; and (4) surfactant. The composition according to the present invention is characterized in that it dissolves in an external phase such as water, artificial gastric fluid and artificial intestinal fluid by controlling the mixing ratio of the components thereby to get the microemulsion form of inner phase diameter of 100 nm or below. The composition according to the present invention can be formulated as the dosage form of a soft capsule, a hard capsule sealed with a gelatin banding at the conjugated portion, or an oral liquid preparation for oral administration.

Abstract: The present invention relates to a pharmaceutical composition containing cyclosporin. More specifically, the present invention relates to a pharmaceutical composition containing cyclosporin, an oil component, a hydrophilic cosurfactant consisting of propylene carbonate or a mixture of propylene carbonate and polyoxyethylene-polyoxypropylene block copolymer, and a surfactant. The composition of the present invention is characterized in that it can be dissolved in an external phase such as water, artificial gastric juice and intestinal juice, etc. to form a self-emulsion with mild stirring and therefore, by appropriately adjusting the constitutional ratio of each component the diameter of particles in the inner phase of the emulsion thus formed can be readily controlled to 100 nm or below. The composition of the present invention can be formulated into the oral preparations such as soft capsules, hard capsules sealed with gelatin bending at the conjugated portion, oral liquid preparations, etc.

Abstract: A process for the isolation of cyclosporin A comprising the steps of: adding a lower alkanol solvent to a culture fluid of a mutant of Tolypocladium inflatum to form a mixture, filtering the mixture to form an extract, transferring the extract to methylene chloride as a solvent therefor, and column chromatographing the resultant product on silica gel.

Abstract: The present invention relates to a process for making a highly productive fusant of Tolypocladium inflatum, a producing strain of cyclosporin A with immunosuppressive properties wherein the selection of the fusant KD461, designed to produce a large amount of cyclosporin A, was made available by the following steps of: developing amino acid-dependent mutants of Tolypocladium inflatum, wild strain isolated from soil, which mutants are induced by UV radiation; conjugating L-valine-dependent and L-leucine-dependent mutants to promote the demand and utility of L-valine and L-leucine, precursors of cyclosporin A, together with an organic nitrogen-source.

Abstract: The present invention relates to a mercaptopyrrolidinyl derivative of the following formula ##STR1## suitable for the preparation of carbapenem compounds.

Abstract: According to the present invention, a process for manufacturing alkali metal salt of clavulanic acid wherein impure clavulanic acid in aqueous solution is extracted by a solvent mixture of ketone and alkyl acetate under acidic condition, treated in a conventional manner, and a solution of alkali metal salt of alkanoic acid dissolved in ketone or alkanol solvent is added to obtain pure alkali metal salt of clavulanic acid is provided.Since the process according to the present invention omits a step of formation of amine salt, an economic and simple method for manufacturing alkali metal salt of clavulanic acid in a high yield without excessive use of solvent is provided.

Abstract: The present invention relates to 2-(2-substituted pyrrolidin-4-yl)-thio-carbapenem derivatives and pharmaceutically acceptable salts thereof, to a process for preparing the derivatives, an intermediate compound for preparing the derivatives, an antibacterial composition containing the derivatives, and use of the derivatives as an antibacterial agent.

Abstract: The present invention relates to a cyclosporin-containing powder composition which comprises cyclosporin, a non-ionic hydrophilic surfactant and a porous carrier. In addition, the present invention relates to a method for preparing the cyclosporin-containing powder composition which comprises dissolving cyclosporin and a non-ionic hydrophilic surfactant in an organic solvent, adding a porous carrier to the resulting solution and then evaporating the organic solvent from the mixture. The powder composition of the present invention is stable and does not require a special manufacturing technique when it is formulated. In addition, since the powder composition of the present invention does not contain an organic solvent, the necessity of a special package is excluded. Furthermore, the composition of the present invention provides an improved bioavailability which results in decrease of a single dosage, and therefore, can contribute to the alleviation of the side effects associated with cyclosporin.